一种西地那非类似物的合成工艺研究

目的 探讨合成一种西地那非类似物的新方法.方法 设计以WG 001-01-08和五硫化二磷为原料,经过硫化得到目标化合物（一种西地那非类似物）的合成路线,并以收率和杂质为指标考察反应试剂、反应温度、加料顺序对反应的影响.结果 成功制备了目标化合物,收率为90％；较佳反应条件为以4-甲基吡啶为溶剂,120℃反应4h,先加WG001-01-08后加五硫化二磷.结论 新方法收率较高,杂质少,反应条件温和,适合工业化生产.

Study on the synthesis technology of sildenafil analogues

Objective To explore a new technology for synthesis of sildenafil analogues. Methods The synthesis route of sildenafil analogues was prepared by the steps of vulcanization from the starting material WG001-01-08 and phos- phorus pentasulfide. The effects of reaction reagent and reaction temperature and feeding order on the yield and impu- rity of sildenafil analogues were studied. Results It was synthesized successfully, the yield was 90%. Optimal reaction condition was as follows： solvent was 4-methylpyridine, reaction temperature was 120~E for 4 h ,and feeding order was WGO01-01-08 and phosphorus pentasulfide. Conclusion The method is characterized with high yield,low impurity and moderate reaction condition. It is suitable for industrial production.